GS-443902 trisodium (GS-441524 triphosphate trisodium) is a potent viralRNA-dependent RNA-polymerases (RdRp)inhibitor withIC₅₀s of 1.1 μM, 5 μM forRSVRdRp andHCVRdRp, respectively. GS-443902 trisodium is the active triphosphate metabolite of Remdesivir (GS-5734)^[1][2].

IC50: 1.1 μM (RSV RdRp) and 5 μM (HCV RdRp)^[1][2]

In a continuous 72 h incubation of 1 μM Remdesivir (GS-5734), the GS-443902 trisodium (GS-441524 triphosphate trisodium; Remdesivir metabolite trisodium) level is measured at 2, 24, 48 and 72 h, and reaches a C_maxof 300, 110, and 90 pmol/million cells in macrophages, HMVEC, and HeLa cells lines respectively^[1].
GS-443902 trisodium (compound 8a) is a triphosphates (TP) derivative^[2].
GS-443902 trisodium (NTP; 0.01, 0.1, 1, 10, 100 μM) inhibits RSV RdRp-catalysed RNA synthesis by incorporating into the nascent viral RNA transcript and causing its premature termination. GS-5734 selectively inhibits EBOV replication by targeting its RdRp and inhibiting viral RNA synthesis following efficient intracellular conversion to GS-443902 sodium^[3].

Remdesivir (GS-5734; 10 mg kg; i.v.) rapidly distributes into peripheral blood mononuclear cells (PBMCs), and efficient conversion to GS-443902 trisodium (Remdesivir metabolite trisodium; NTP) is apparent within 2 h of dose administration in rhesus monkeys. In PBMCs, GS-443902 trisodium represents the predominant metabolite and is persistent with a t_1/2of 14 h and levels required for >50% virus inhibition for 24 hours^[3].

597.15

Solid

C₁₂H₁₃N₅Na₃O₁₃P₃

1355050-21-3

瑞德西韦代谢物三钠盐

Room temperature in continental US; may vary elsewhere.

-80°C, protect from light, stored under nitrogen

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

H₂O : 33.33 mg/mL(55.82 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： PBS

  Solubility: 50 mg/mL (83.73 mM); Clear solution; Need ultrasonic